ABT-724 je lek koji deluje kao dopaminski agonist. On je selektivan za D4 podtip.[5] ABT-724 je razvijen kao mogući lek za impotenciju,[6] mada zbog slabe oralne biodostupnosti verovatno neće naći kliničku primenu.[7] On se koristi u naučnim istraživanjima funkcije D4 receptora.[8][9]

ABT-724
(IUPAC) ime
2-(4-piridin-2-ilpiperazin-1-ilmetil)-1H-benzimidazol
Klinički podaci
Identifikatori
CAS broj 70006-24-5
ATC kod nije dodeljen
PubChem[1][2] 5025739
ChemSpider[3] 4204515
ChEMBL[4] CHEMBL440687 DaY
Hemijski podaci
Formula C17H19N5 
Mol. masa 293,366 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Reference uredi

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. Brioni JD, Moreland RB, Cowart M, Hsieh GC, Stewart AO, Hedlund P, Donnelly-Roberts DL, Nakane M, Lynch JJ, Kolasa T, Polakowski JS, Osinski MA, Marsh K, Andersson KE, Sullivan JP (April 2004). „Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats”. Proceedings of the National Academy of Sciences of the United States of America 101 (17): 6758–63. DOI:10.1073/pnas.0308292101. PMC 404118. PMID 15087502. 
  6. Cowart M, Latshaw SP, Bhatia P, Daanen JF, Rohde J, Nelson SL, Patel M, Kolasa T, Nakane M, Uchic ME, Miller LN, Terranova MA, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino BR, Lynch JJ, Sullivan JP, Hsieh GC, Moreland RB, Brioni JD, Stewart AO (July 2004). „Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction”. Journal of Medicinal Chemistry 47 (15): 3853–64. DOI:10.1021/jm030505a. PMID 15239663. 
  7. Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO (December 2006). „Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction”. Journal of Medicinal Chemistry 49 (25): 7450–65. DOI:10.1021/jm060662k. PMID 17149874. 
  8. Newman-Tancredi A, Heusler P, Martel JC, Ormière AM, Leduc N, Cussac D (May 2008). „Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells”. The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP) 11 (3): 293–307. DOI:10.1017/S1461145707008061. PMID 17897483. 
  9. Marona-Lewicka D, Chemel BR, Nichols DE (April 2009). „Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI”. Psychopharmacology 203 (2): 265–77. DOI:10.1007/s00213-008-1238-0. PMID 18604600. 

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